1. Signaling Pathways
  2. Antibody-drug Conjugate/ADC Related
  3. ADC Linker

Antibody-drug conjugates linker

Antibody-drug conjugates (ADCs) consist of a desirable monoclonal antibody, an active cytotoxic drug and an appropriate linker. An appropriate linker between the antibody and the cytotoxic drug provides a specific bridge, and thus helps the antibody to selectively deliver the cytotoxic drug to tumor cells and accurately releases the cytotoxic drug at tumor sites. In addition to conjugation, the linkers maintain ADCs’ stability during the preparation and storage stages of the ADCs and during the systemic circulation period.

The ADCs currently undergoing clinical evaluation contain linkers are mostly classified into two categories: cleavable and noncleavable. Cleavable linkers rely on processes inside the cell to liberate the toxin, such as reduction in the cytoplasm, exposure to acidic conditions in the lysosome, or cleavage by specific proteases within the cell. Noncleavable linkers require proteolytic degradation of the antibody portion of the ADC for release of the cytotoxic molecule, which will retain the linker and the amino acid by which it was attached to the antibody.

The selection of linker is target dependent, based on the knowledge of the internalization and degradation of the antibody-target antigen complex, and a preclinical in vitro and in vivo activity comparison of conjugates. Moreover, the choice of a linker is also influenced by which cytotoxin is used, as each molecule has different chemical constraints, and frequently the drug structure lends itself to a specific linker.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-156322
    BCN-exo-PEG3-maleimide
    BCN-exo-PEG3-maleimide is an ADC Linker containing 3 PEG units. BCN-exo-PEG3-maleimide contains the lyophilic bidentate macrocyclic ligand BCN, which enables the further synthesis of macrocyclic complexes. In click chemistry, BCN reacts with molecules containing azide groups to form stable triazoles in the absence of catalysts. Its maleimide group (-Maleimide) degrades in aqueous media and has been used in drug delivery studies.
    BCN-exo-PEG3-maleimide
  • HY-152919
    Mal-amide-PEG8-Val-Cit-PAB-OH
    Mal-amide-PEG8-Val-Cit-PAB-OH is a cleavable ADC linker featuring a maleimide, a hydrophilic PEG spacer, a Val-Cit dipeptide, and a PAB functional group. Maleimide is used to covalently bind free thiols on the cysteine residues of proteins. The Val-Cit dipeptide is cleaved by cellular proteases within the cell to allow for efficient payload delivery with the help of the PAB structure.
    Mal-amide-PEG8-Val-Cit-PAB-OH
  • HY-P2376
    Arg-Phe-Asp-Ser
    Arg-Phe-Asp-Ser is a cleavable ADC linker.
    Arg-Phe-Asp-Ser
  • HY-151733
    Fmoc-D-Dbu(N3)-OH
    Fmoc-D-Dbu(N3)-OH is a click chemistry reagent containing an Azide. Fmoc-D-Dbu(N3)-OH is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    Fmoc-D-Dbu(N3)-OH
  • HY-151842
    Fmoc-EDA-N3
    Fmoc-EDA-N3 is a click chemistry reagent containing an azide group. Fmoc-EDA-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    Fmoc-EDA-N3
  • HY-W800622
    Fmoc-PEG4-Val-Cit-PAB-OH
    Fmoc-PEG4-Val-Cit-PAB-OH is an enzyme-cleavable ADC linker featuring a Boc-protected amine, a hydrophilic PEG spacer, and a Val-Cit-PAB dipeptide. The benzylic alcohol on the PAB can be used to attach with reactive groups such as PNP for conjugation with drug payloads. The Fmoc protecting group may be removed with piperidine to reveal a primary amine which may be used in coupling reactions to form amides. The Val-Cit-PAB is cleaved by cellular proteases for efficient release of payloads to the cell.
    Fmoc-PEG4-Val-Cit-PAB-OH
  • HY-151816
    alpha-Man-TEG-N3
    alpha-Man-TEG-N3 is a click chemistry reagent containing an azide group. alpha-Man-TEG-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    alpha-Man-TEG-N3
  • HY-151780
    Fmoc-L-Dap(Pentynoyl)-OH
    Fmoc-L-Dap(Pentynoyl)-OH is a click chemistry reagent containing an azide group. Fmoc-L-Dap(Pentynoyl)-OH serves as an amino acid building block for introducing alkyne functions into peptide sequences by standard Fmoc/tBu protocols. The alkyne residue can be engaged for copper catalyzed click reaction with organic azides or with tetrazines for copper-free conjugations. Fmoc-L-Dap(Pentynoyl)-OH is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Fmoc-L-Dap(Pentynoyl)-OH
  • HY-41064
    N-Boc-N-methyl-D-Valaldehyde
    N-Boc-N-methyl-D-Valaldehyde is an ADC linker with a BOC protecting group.
    N-Boc-N-methyl-D-Valaldehyde
  • HY-151790
    Alkyne-SS-COOH
    Alkyne-SS-COOH is a click chemistry reagent containing an alkyne group. Alkyne-SS-COOH can be used for the research of various biochemical.
    Alkyne-SS-COOH
  • HY-151721
    H-D-Orn(N3)-OH hydrochloride
    H-D-Orn(N3)-OH hydrochloride is a click chemistry reagent containing an azide group. Click chemistry has great potential for use in binding between nucleic acids, lipids, proteins, and other molecules, and has been used in many research fields because of its beneficial characteristics, including high yield, high specificity, and simplicity. It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
    H-D-Orn(N3)-OH hydrochloride
  • HY-W800814
    Azido-PEG8-Amido-Val-Cit-PAB
    Azido-PEG8-Amido-Val-Cit-PAB is a cleavable ADC linker. The Val-Cit will specifically be cleaved by Cathepsin B. As this enzyme is only present in the lysosome, the ADC payload will be released only in the cell. Azido will react with DBCO, BCN or other alkyne groups through click chemistry. PEG spacer increases aqueous solubility. Reagent grade, for research purpose.
    Azido-PEG8-Amido-Val-Cit-PAB
  • HY-151814
    (2S,4S)-Fmoc-L-Pro(4-NHPoc)-OH
    (2S,4S)-Fmoc-L-Pro(4-NHPoc)-OH is a click chemistry reagent containing an azide group.
    (2S,4S)-Fmoc-L-Pro(4-NHPoc)-OH
  • HY-W540192
    SCO-PEG2-Maleimide
    SCO-PEG2-Maleimide is an ADC Linker containing 3 PEG units. SCO-PEG2-Maleimide can be used as a copper-free click chemical reagent for catalyst-free click reactions. Its maleimide group (-Maleimide) degrades in aqueous media and has been used in drug delivery studies.
    SCO-PEG2-Maleimide
  • HY-164273
    Azidoacetyl-Val-Cit-PAB-OH
    Azidoacetyl-Val-Cit-PAB-OH is a cleavable ADC linker.
    Azidoacetyl-Val-Cit-PAB-OH
  • HY-151796
    DACN(Ms,Ns)
    DACN(Ms,Ns) is a click chemistry reagent containing a cyclic alkyne group.
    DACN(Ms,Ns)
  • HY-133540G
    Maleimide-DOTA (GMP)
    Maleimide-DOTA (Maleimido-mono-amide-DOTA) (GMP) is Maleimide-DOTA (HY-133540) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Maleimide-DOTA is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
    Maleimide-DOTA (GMP)
  • HY-151764A
    N3-D-Orn(Boc)-OH (CHA)
    N3-D-Orn(Boc)-OH (CHA) is a Boc-protected pentanoic amino acid derivative, can be used as a click chemistry reagent and has been used to synthesis antibody-drug conjugates (ADC). It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
    N3-D-Orn(Boc)-OH (CHA)
  • HY-151815
    beta-Lac-TEG-N3
    beta-Lac-TEG-N3 is a click chemistry reagent containing an azide group. beta-Lac-TEG-N3 can be used for the research of various biochemical. It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
    beta-Lac-TEG-N3
  • HY-151709A
    N3-L-Cit-OH (DCHA)
    N3-L-Cit-OH DCHA is a click chemistry reagent containing an azide group. N3-L-Cit-OH DCHA can be used to construct peptidomimetic ADC linkers using Click-chemistry. It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
    N3-L-Cit-OH (DCHA)

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